JDTic (2HCl) Struktur

JDTic (2HCl)

Bezeichnung:JDTic (2HCl)

CAS-Nr785835-79-2

Englisch Name:JDTic (2HCl)

CBNumberCB02624189

SummenformelC28H40ClN3O3

Molgewicht502.1

MOL-Datei785835-79-2.mol

JDTic (2HCl) physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	Soluble in DMSO
Aggregatzustand	Powder
Farbe	White to off-white

JDTic (2HCl) Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
jdtic is a selective inhibitor of kappa opioid receptor with ic50 value of 0.02nm [1].jdtic is one of the kappa opioid receptor selective antagonists. these antagonists are thought as potential pharmacotherapies for addiction, anxiety disorders, depression, psychosis disorders and obesity. because of the unique structural feature of jdtic, it is more selective and potent for kor activity than other kor antagonists. jdtic is shown to block the antinociceptive response of nicotine in the tail-flick test with a dose-dependent manner. it (8 mg/kg) can also block the nicotine withdrawal signs in mice via effecting the expression of a cpa associated with nicotine withdrawal. additionally, jdtic is also reported to decrease the number of somatic withdrawal signs in morphine-dependent rats [2,3].
target
kappa opioid receptor
Einzelnachweise
[1] michael p. hedrick, palak gosalia, kelin li, kevin frankowski, shenghua shi, thomas e. prisinzano, frank schoenen, jeffrey aubé, ying su, s. vasile, eduard sergienko, wilson gray, santosh hariharan, loribelle milan, susanne heynen-genel, bryan l. roth, jon evans, vincent setola, thomas d.y. chung, marc caron, laura m. bohn and lawrence s. barak. antagonist for the kappa opioid receptor. molecular libraries. 2011 jun: 1-32.
[2] scott p. runyon, lawrence e. brieaddy, s. wayne mascarella, james b. thomas, hernán a. navarro, james l. howard, gerald t. pollard, and f. ivy carroll. analogues of (3r)-7-hydroxy-n-[(1s)-1-{[(3r,4r)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide(jdtic). synthesis and in vitro and in vivo opioid receptor antagonist activity. j med chem. 2010 july, 53(14): 5290–5301.
[3] k. j. jackson, frank ivy carroll, s. s. negus and m. i. damaj. effect of the selective kappa-opioid receptor antagonist jdtic on nicotine antinociception, reward, and withdrawal in the mouse. psychopharmacology (berl). 2010 june, 210(2): 285–294.

JDTic (2HCl) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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